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Apoptosis——TNF Receptor

Tumor necrosis factor (TNF) is a major mediator of apoptosis as well as inflammation and immunity, and it has been implicated in the pathogenesis of a wide spectrum of human diseases, including sepsis, diabetes, cancer, osteoporosis, multiple sclerosis, rheumatoid arthritis, and inflammatory bowel diseases.

TNF-α is a 17-kDa protein consisting of 157 amino acids that is a homotrimer in solution. In humans, the gene is mapped to chromosome 6. Its bioactivity is mainly regulated by soluble TNF-α–binding receptors. TNF-α is mainly produced by activated macrophages, T lymphocytes, and natural killer cells. Lower expression is known for a variety of other cells, including fibroblasts, smooth muscle cells, and tumor cells. In cells, TNF-α is synthesized as pro-TNF (26 kDa), which is membrane-bound and is released upon cleavage of its pro domain by TNF-converting enzyme (TACE).

Many of the TNF-induced cellular responses are mediated by either one of the two TNF receptors, TNF-R1 and TNF-R2, both of which belong to the TNF receptor super-family. In response to TNF treatment, the transcription factor NF-κB and MAP kinases, including ERK, p38 and JNK, are activated in most types of cells and, in some cases, apoptosis or necrosis could also be induced. However, induction of apoptosis or necrosis is mainly achieved through TNFR1, which is also known as a death receptor. Activation of the NF-κB and MAPKs plays an important role in the induction of many cytokines and immune-regulatory proteins and is pivotal for many inflammatory responses.

Apoptosis——TNF Receptor(91)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM8848 (Rac)-Benpyrine

(Rac)-Benpyrine,Benpyrine 的外消旋体,是一种有效的具有口服活性的 TNF-α 抑制剂。(Rac)-Benpyrine 可用于 TNF-α 介导的炎症和自身免疫性疾病的研究。

1333714-43-4 99%
KE7633 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea 2379727-88-3 ≥95%
KE5163 11-Hydroxytephrosin 72458-85-6 ≥95%
KE7044 3,5-Dicaffeoyl-epi-quinic acid 879305-14-3 ≥95%
KE6718 7-O-Methylmorroniside 119943-46-3 ≥95%
KE4485 8alpha-Hydroxyhirsutinolide 1394156-45-6 ≥95%
KM17155 Adalimumab

Adalimumab 是一种人源的单克隆 IgG1 抗体,靶向肿瘤坏死因子α (TNF-α)。

331731-18-1 99%
KM6475 Apratastat

Apratastat 是一种口服活性,有效且可逆的肿瘤坏死因子-α 转换酶 TACE 和基质金属蛋白酶 MMPs 的双重抑制剂。Apratastat 可以在体外,离体和体内有效抑制 TNF-α 的释放,体外和离体的 IC50 分别为 144 ng/mL和 81.7 ng/mL。

287405-51-0 99%
KM2800 Apremilast

Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂,IC50 为 74 nM。Apremilast 抑制脂多糖 (LPS) 释放 TNF-α,IC50 为 104 nM。

608141-41-9 99%
KM11185 Apremilast D5

Apremilast D5 (CC-10004 D5) 是一种 Apremilast 氘代物。Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂,IC50 为 74 nM。Apremilast 抑制脂多糖 (LPS) 释放 TNF-α,IC50 为 104 nM。

1258597-47-5
KE5311 Arteannuin N 207446-92-2 ≥95%
KE6884 Artocarpin 7608-44-8 ≥95%
KM19196 Astilbin

Astilbin 是一种黄酮类化合物,可增强 NRF2 活化。Astilbin 还抑制 TNF-α 表达和 NF-κB 活化。

29838-67-3 98%
KM2750 AX-024

AX-024 是一种口服可利用的,首创的 TCR-Nck 相互作用抑制剂,可选择性地抑制 TCR 触发的 T 细胞活化,IC50 值为 1 nM。AX-024 通过靶向 SH3 结构域调节细胞信号传导。AX-024 具有低毒、高效、高选择性的特点。AX-024 有效抑制白细胞介素-6 (IL-6),肿瘤坏死因子-α (TNFα),干扰素-γ (IFN-γ),IL-10IL-17A 的产生。

1370544-73-2 ≥98%
KM7261 AX-024 hydrochloride

AX-024 hydrochloride 是一种口服可利用的,首创的 TCR-Nck 相互作用抑制剂,可选择性地抑制 TCR 触发的 T 细胞活化,IC50 值为 1 nM。AX-024 hydrochloride 通过靶向 SH3 结构域调节细胞信号传导。AX-024 hydrochloride 具有低毒、高效、高选择性的特点。AX-024 hydrochloride 有效抑制白细胞介素-6 (IL-6),肿瘤坏死因子-α (TNFα),干扰素-γ (IFN-γ),IL-10IL-17A 的产生。

1704801-24-0 99%
KM8627 Benpyrine

Benpyrine 是一种高度特异性的具有口服活性的 TNF-α 抑制剂,KD 值为 82.1 μM。Benpyrine 与 TNF-α 紧密结合并阻断其与 TNFR1 的相互作用,IC50 值为 0.109 µM。Benpyrine 可用于 TNF-α 介导的炎症和自身免疫性疾病的研究。

2550398-89-3 99%
KM17793 Bioymifi

Bioymifi 是一种有效的 TRAIL 受体 DR5 激活剂,与DR5的胞外结构域 (ECD) 结合,Kd 为 1.2 μM,Bioymifi 可作为单一的诱导剂诱导 DR5 的聚集,导致细胞凋亡。

1420071-30-2 ≥98%
KE7632 BMS-561392 611227-74-8 ≥95%
KM4853 C 87

C 87 是一种新型小分子 TNFα 抑制剂; 高效抑制 TNFα 诱导的细胞毒性,IC50 值为 8.73 μM。

332420-90-3 98%
KM8817 C25-140

C25-140 是一种首创的,具有口服活性和一定选择性的 TRAF6-Ubc13 相互作用的抑制剂,直接与 TRAF6 结合,阻断 TRAF6 和 Ubc13 的相互作用,从而降低 TRAF6 活性,降低 NF-κB 的活性,并对抗自身免疫。

1358099-18-9 99%
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